CN107549803B - Effervescent tablet containing alpha-ketoacid and preparation method thereof - Google Patents

Effervescent tablet containing alpha-ketoacid and preparation method thereof Download PDF

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CN107549803B
CN107549803B CN201710854945.3A CN201710854945A CN107549803B CN 107549803 B CN107549803 B CN 107549803B CN 201710854945 A CN201710854945 A CN 201710854945A CN 107549803 B CN107549803 B CN 107549803B
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effervescent tablet
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keto acid
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何连顺
米造吉
李斌水
马静
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Jing Jing Pharmaceutical Co ltd
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Abstract

The invention relates to the technical field of medicines, and particularly discloses an effervescent tablet containing alpha-keto acid and a preparation method thereof. The effervescent tablet containing the alpha-ketoacid comprises the following components in parts by weight: 60-100 parts of alpha-keto acid; alpha-ketonate 230-410 parts; 20-100 parts of trehalose; 10-60 parts of L-glutamine; 1-10 parts of magnesium aminoacetate; 1-10 parts of carnosine zinc; 1-10 parts of lysine; 1-10 parts of arginine; 5-60 parts of flavoring agent. The effervescent tablet containing the alpha-ketoacid provided by the invention takes the specific alpha-ketoacid, the specific alpha-ketoacid salt and the specific amino acid as main components, and the components are compatible, so that the supply of energy and the amino acid is effectively improved, the body fluid balance is promoted, the effervescent tablet containing the alpha-ketoacid can be used as a health-care product, the symptoms of soreness, weakness, dizziness and the like of the lumbar muscles of sub-health people are relieved, and meanwhile, trehalose and a flavor are added into the effervescent tablet containing the alpha-ketoacid, the mouthfeel of the effervescent tablet is improved, a user can quickly get rid of the sub-health state, and the recovery of the body function is facilitated.

Description

Effervescent tablet containing alpha-ketoacid and preparation method thereof
Technical Field
The invention relates to the technical field of medicines, in particular to an effervescent tablet containing alpha-keto acid and a preparation method thereof.
Background
Alpha-keto acids are keto acids with two carboxyl groups directly adjacent to each other, pyruvic acid being the simplest alpha-keto acid. Pyruvic acid can be decomposed into acetaldehyde and carbon dioxide in the process of alcoholic fermentation. Can also be decomposed into acetyl coenzyme A and sulfur dioxide under the action of enzyme. A similar reaction occurs in the tricarboxylic acid cycle. Another typical reaction is a transamination reaction, in which an α -keto acid acquires an amino group, while a hub amino acid loses an amino group without releasing ammonia. By this reaction pyruvate can be converted to alanine, oxaloacetate (which is both an alpha-keto acid and a beta-keto acid) to aspartate, and a-ketoglutarate to the methionine. The alpha-keto acid generated after deamination of the amino acid can be further metabolized to generate non-essential amino acids by amination, converted into glycogenic amino acids or ketogenic amino acids, or directly oxidized by tricarboxylic acid cycle and oxidative phosphorylation to generate CO2And water, and release energy for life activities.
The ketoacid mainly supplements branched chain amino acids, compared with a pure low-protein diet, the ketoacid can supply enough essential amino acids, energy and essential nutrients, has double functions of reducing proteinuria and avoiding malnutrition, supplements the limitation of pure low-protein supplementation, does not have the risk of causing malnutrition, maintains the renal function to the maximum extent, can obviously improve sub-health symptoms such as hypodynamia, waist soreness and backache, dizziness and the like, and is a kidney tonifying strong health care product with high applicability. At present, the effervescent tablet health-care product mostly has single amino acid compatibility and single alpha-ketoacid compatibility and poor taste, is targeted to the sick people as a medicament, and cannot be used as a health-care product for sub-healthy middle-aged and young people and middle-aged and old people.
Disclosure of Invention
Aiming at the problems of poor taste, single applicable crowd and the like caused by single compatibility of amino acid and alpha-keto acid in the effervescent tablet containing alpha-keto acid in the prior art, the invention provides the effervescent tablet containing the alpha-keto acid and the preparation method thereof.
In order to achieve the purpose of the invention, the embodiment of the invention adopts the following technical scheme:
an effervescent tablet containing alpha-ketoacid comprises the following components in parts by weight:
Figure BDA0001413448150000021
wherein the alpha-keto acid comprises alpha-ketoglutaric acid, alpha-hydroxymethionine; the alpha-ketoacid salt comprises alpha-ketovaline calcium, alpha-ketoleucine calcium, alpha-ketoisoleucine calcium, alpha-ketoacid calcium and alpha-ketophenylalanine calcium.
Compared with the prior art, the effervescent tablet containing alpha-keto acid provided by the invention takes specific alpha-keto acid (alpha-ketoglutaric acid and alpha-hydroxymethionine), specific alpha-ketonic acid salt (alpha-ketovaline calcium, alpha-ketoleucine calcium, alpha-ketoisoleucine calcium, alpha-keto acid calcium and alpha-ketophenylalanine calcium) and specific amino acid (lysine and arginine) as main components, and the components are compatible to effectively improve the supply of energy and amino acid and promote the balance of body fluid, so that the effervescent tablet containing alpha-keto acid can be used as a health-care product to relieve symptoms of waist muscle soreness, weakness, dizziness and the like of sub-healthy people, and the applicable population of the product (no longer limited to the sick people) is improved. Meanwhile, the trehalose and the flavor agent are added into the effervescent tablet containing the alpha-ketonic acid, so that the taste of the effervescent tablet can be improved, the effervescent tablet containing the alpha-ketonic acid can be suitable for different people, a user can quickly get rid of a sub-health state, and the recovery of body functions is facilitated.
Furthermore, the invention also provides a preparation method of the effervescent tablet containing the alpha-keto acid. The preparation method at least comprises the following steps:
(1) mixing the trehalose, alpha-keto acid salt, L-glutamine, aminoacetic acid and carnosine zinc, and then carrying out wet granulation to obtain a complex A;
(2) mixing lysine, arginine and a flavoring agent, and then granulating by a wet method to obtain a complex B;
(3) respectively taking part of the complex A and the complex B according to the same weight ratio to prepare aqueous solution, adding an alkaline regulator into the aqueous solution, regulating the pH value to 7.35-7.45, and recording the proportion of the alkaline regulator to the complex A and the complex B;
(4) mixing the rest complex A, the rest complex B and an alkaline regulator according to the proportion in the step (3) to obtain a mixed material;
(5) uniformly spraying a binding agent with the weight of 2-7% of the total weight of the mixed material into the mixed material, and tabletting to obtain the effervescent tablet containing the alpha-ketoacid.
Compared with the prior art, the preparation method of the effervescent tablet containing the alpha-ketoacid, provided by the invention, has the advantages of simple process, convenience in operation, greenness and environmental friendliness, enables the components to be more uniform through multiple mixing, and can quickly prepare the effervescent tablet health-care product taking the alpha-ketoacid as the main component.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is further described in detail with reference to the following embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.
The embodiment of the invention provides an effervescent tablet containing alpha-keto acid. The effervescent tablet comprises the following components in parts by weight:
Figure BDA0001413448150000041
wherein the alpha-keto acid comprises alpha-ketoglutaric acid, alpha-hydroxymethionine; the alpha-ketoacid salt comprises alpha-ketovaline calcium, alpha-ketoleucine calcium, alpha-ketoisoleucine calcium, alpha-ketoacid calcium and alpha-ketophenylalanine calcium.
Preferably, the alpha-keto acid comprises the following components in parts by weight:
20-30 parts of alpha-ketoglutaric acid;
40-70 parts of alpha-hydroxymethionine; and/or
The alpha-ketonic acid salt comprises the following components in parts by weight:
Figure BDA0001413448150000051
the main component of the effervescent tablet containing alpha-keto acid is formed by matching various alpha-keto acid and alpha-keto acid salt with amino acid.
Preferably, the effervescent tablet containing the alpha-keto acid further comprises an alkaline regulator, a binder; wherein the dosage of the alkaline regulator is determined by pH, and the pH of the system is regulated to 7.35-7.45; the dosage of the adhesive is 2-7% of the total weight of the other components, which is helpful for tabletting treatment and the effervescent tablet containing the alpha-ketoacid is obtained.
Further preferably, the alkaline regulator is a mixture of sodium bicarbonate and sodium carbonate, wherein the mass ratio of the sodium bicarbonate to the sodium carbonate is (0.3-0.5): 1, the pH of the system is regulated, and the pH is controlled to be 7.35-7.45 and is matched with the pH of the environment in the human body.
Preferably, the effervescent tablets containing the alpha-keto acid have a specification of 2 g/tablet and 4 g/tablet, so as to be convenient for different people to use.
The effervescent tablet containing alpha-keto acid provided by the embodiment of the invention takes various alpha-keto acids, alpha-keto acid salts and amino acids as main components, the taste of the effervescent tablet is improved by adding trehalose and flavoring agents, and the effervescent tablet is stronger in pertinence on energy and amino acid supplementation, body fluid balance and relieving symptoms such as lumbar muscle soreness, weakness, dizziness and the like of sub-health people aiming at different people, so that a user can quickly get rid of a sub-health state, and the recovery of body functions is facilitated.
The invention further provides a preparation method of the effervescent tablet containing the alpha-keto acid on the premise of providing the effervescent tablet containing the alpha-keto acid.
In one embodiment, the preparation method at least comprises the following steps:
(1) mixing the trehalose, alpha-keto acid salt, L-glutamine, aminoacetic acid and carnosine zinc, and then carrying out wet granulation to obtain a complex A;
(2) mixing lysine, arginine and a flavoring agent, and then granulating by a wet method to obtain a complex B;
(3) respectively taking part of the complex A and the complex B according to the same weight ratio to prepare aqueous solution, adding an alkaline regulator into the aqueous solution, regulating the pH value to 7.35-7.45, and recording the proportion of the alkaline regulator to the complex A and the complex B;
(4) mixing the rest complex A, the rest complex B and an alkaline regulator according to the proportion in the step (3) to obtain a mixed material;
(5) uniformly spraying a binding agent with the weight of 2-7% of the total weight of the mixed material into the mixed material, and tabletting to obtain the effervescent tablet containing the alpha-ketoacid.
The above preparation process is further explained below:
preferably, in the steps (1) and (2), the mixing treatment is realized by a mixer; the mixer is a double-cone or V-shaped cone mixer, and materials are fully mixed.
Preferably, the wet granulation is realized by a granulator, and the particle size is sieved by a screen to obtain the compound A and the compound B with ideal particle sizes.
Further preferably, the water for wet granulation is purified water or deionized water, and the water temperature is 15-25 ℃.
Preferably, the particle size of the complex A is less than or equal to 120 mu m; the particle size of the complex B is less than or equal to 120 mu m, which is beneficial to the later mixing and tabletting treatment to obtain the effervescent tablet with uniform components.
Preferably, the mass fraction of the aqueous solution is 4%.
Preferably, in the mixed material in the step (4), the total weight percentage of the alpha-ketonic acid and the alpha-ketonic acid salt is 40-70% based on 100% of the total weight of the mixed material.
The method has the advantages of simple preparation process, convenient operation, environmental protection, more uniform components through multiple mixing, and capability of quickly preparing the effervescent tablet health-care product taking the alpha-keto acid as the main component.
To better illustrate the effervescent tablet containing an α -keto acid and the method for preparing the same provided in the examples of the present invention, further examples are provided below.
Example 1
The preparation method of the effervescent tablet containing alpha-keto acid comprises the following steps:
(1) in a clean room C-level area, controlling the humidity to be less than or equal to 45 percent, controlling the temperature to be 23-25 ℃, weighing 11 substances in total, namely 4.0kg of trehalose, 2.0kg of alpha-ketoglutaric acid, 7.5kg of alpha-ketovaline calcium, 4.5kg of alpha-hydroxymethionine, 7.5kg of alpha-ketoleucine calcium, 4.0kg of alpha-ketoisoleucine calcium, 3.0kg of alpha-keto acid calcium, 3.0kg of alpha-ketophenylalanine calcium, 1.0kg of L-glutamine, 0.5kg of magnesium aminoacetate and 0.5kg of carnosine zinc, uniformly mixing the substances in a double-cone mixer by weight, carrying out aqueous phase wet granulation, sieving the mixture by using a granulator, and selecting a 120 mu m sieve to prepare an alpha-keto acid complex A for standby use, wherein the total weight is 38.7 kg;
(2) meanwhile, 1.0kg of lysine, 1.0kg of arginine and 1.5kg of pineapple essence flavoring agent are subjected to wet granulation in another mixer, and the mixture passes through a granulator and a 120 mu m screen to prepare an alpha-keto acid complex B for later use, and 3.7kg of the alpha-keto acid complex B is weighed;
(3) taking 38.7g of alpha-keto acid complex A and 3.7g of complex B, preparing 1L of aqueous solution with the concentration of about 4%, adding an alkaline regulator into the aqueous solution, detecting the pH of the aqueous solution, regulating the pH to 7.35 by using sodium bicarbonate/sodium carbonate serving as the alkaline regulator, recording the weight of the alkaline regulator to be 4.9g, and determining the proportion of the alkaline regulator to the complex A and the complex B;
(4) adding the alpha-ketonic acid complex A, the complex B and the alkaline regulator into a mixer according to the proportion of the alkaline regulator to the complex A and the complex B for mixing, weighing 47.3kg of uniformly mixed powder, detecting two indexes of the total content and the pH of the alpha-ketonic acid according to a sampling method, detecting that the total content of the alpha-ketonic acid is 60.33 percent and the pH is 7.39, meeting the internal control index, uniformly spraying an adhesive accounting for 2 percent of the total weight of the powder into the powder for tabletting to obtain the effervescent tablet containing the alpha-ketonic acid with the specification of 4 g/tablet, packaging 20 tablets/tube, automatically setting 10 tubes of the tubular effervescent tablet as one box, packaging into 56 boxes, and packaging with the yield of 94.7 percent.
Example 2
The preparation method of the effervescent tablet containing alpha-keto acid comprises the following steps:
(1) in a clean room C-level area, controlling the humidity to be less than or equal to 45 percent, controlling the temperature to be 23-25 ℃, weighing 8.0kg of trehalose, 2.0kg of alpha-ketoglutaric acid, 8.0kg of alpha-ketovaline calcium, 5.5kg of alpha-hydroxymethionine, 6.5kg of alpha-ketoleucine calcium, 5.5kg of alpha-ketoisoleucine calcium, 3.0kg of alpha-keto acid calcium, 3.0kg of alpha-ketophenylalanine calcium, 1.0kg of L-glutamine, 1.0kg of magnesium aminoacetate and 0.5kg of carnosine zinc by weight, uniformly mixing in a double-cone mixer, carrying out aqueous phase wet granulation, passing through a granulator, selecting a 120 mu m screen mesh for screening, and preparing an alpha-keto acid complex A for standby use, wherein the total weight is 45.0 kg;
(2) meanwhile, 1.0kg of lysine, 1.0kg of arginine and 3.5kg of strawberry essence are subjected to wet granulation in another mixer, and the mixture passes through a granulator and a 120-micron screen to prepare a complex B for later use, and 6.9kg of the complex B is weighed;
(3) preparing 1.0L of an aqueous solution with the concentration of about 4% by taking 35g g of the alpha-keto acid complex A and 4.9g of the complex B, adding an alkaline regulator into the aqueous solution, detecting the pH value of the aqueous solution, regulating the pH value to 7.45 by using sodium bicarbonate/sodium carbonate serving as the alkaline regulator, recording the weight of the alkaline regulator to be 7.6g, and determining the proportion of the alkaline regulator to the complex A and the complex B;
(4) adding 45.0kg, 6.9kg and 7.6kg of alpha-ketonic acid A complex, alpha-B complex and alkaline regulator into a mixer according to the proportion of the alkaline regulator to the complex A and the complex B for mixing, weighing 59.4kg of uniformly mixed powder, detecting two indexes of the total content and the pH value of the alpha-ketonic acid according to a sampling method, detecting that the total content of the alpha-ketonic acid is 49.1 percent and the pH value is 7.45, meeting the internal control index, uniformly spraying an adhesive accounting for 2 percent of the total weight of the powder into the powder for tabletting to obtain effervescent tablets with the specification of 4 g/tablet, and packaging 20 tablets/tube. The tube-packed effervescent tablets are automatically set to count 10 tubes into one box, and are packaged into 72 boxes, and the packaging yield is 96.9%.
Example 3
The preparation method of the effervescent tablet containing alpha-keto acid comprises the following steps:
(1) in a clean room C-level area, controlling the humidity to be less than or equal to 45 percent, controlling the temperature to be 23-25 ℃, weighing 11 substances in total, namely 4.0kg of trehalose, 2.0kg of alpha-ketoglutaric acid, 7.5kg of alpha-ketovaline calcium, 4.5kg of alpha-hydroxymethionine, 7.5kg of alpha-ketoleucine calcium, 4.0kg of alpha-ketoisoleucine calcium, 3.0kg of alpha-keto acid calcium, 3.0kg of alpha-ketophenylalanine calcium, 1.0kg of L-glutamine, 0.5kg of magnesium aminoacetate and 0.5kg of carnosine zinc, uniformly mixing the substances in a double-cone mixer by weight, carrying out aqueous phase wet granulation, sieving the mixture by using a granulator, and selecting a 120 mu m sieve to prepare an alpha-keto acid complex A for standby use, wherein the total weight is 38.7 kg;
(2) meanwhile, 1.0kg of lysine, 1.0kg of arginine and 1.5kg of pineapple essence flavoring agent are subjected to wet granulation in another mixer, and the mixture passes through a granulator and a 120 mu m screen to prepare an alpha-keto acid complex B for later use, and 3.7kg of the alpha-keto acid complex B is weighed;
(3) taking 38.7g of alpha-keto acid complex A and 3.7g of complex B, preparing 1L of aqueous solution with the concentration of about 4%, adding an alkaline regulator into the aqueous solution, detecting the pH of the aqueous solution, regulating the pH to 7.35 by using sodium bicarbonate/sodium carbonate serving as the alkaline regulator, recording the weight of the alkaline regulator to be 4.9g, and determining the proportion of the alkaline regulator to the complex A and the complex B;
(4) adding the alpha-ketonic acid complex A, the complex B and the alkaline regulator into a mixer according to the proportion of the alkaline regulator to the complex A and the complex B for mixing, weighing 30kg of uniformly mixed powder, detecting two indexes of the total content and the pH of the alpha-ketonic acid according to a sampling method, detecting that the total content of the alpha-ketonic acid is 60.33 percent and the pH is 7.39, meeting the internal control index, uniformly spraying an adhesive accounting for 2 percent of the total weight of the powder into the powder for tabletting to obtain the effervescent tablet containing the alpha-ketonic acid with the specification of 2 g/tablet, packaging 10 tablets/pipe, automatically setting the number of 10 pipes of the effervescent tablet in the pipe as one box, packaging the effervescent tablet in the pipe into 143 boxes, and packaging the effervescent tablet with the yield of 95.3 percent.
The data show that the preparation method of the effervescent tablet containing the alpha-ketoacid provided by the embodiment of the invention has the advantages of simple process, convenient operation, environmental protection and capability of quickly preparing the effervescent tablet health-care product taking the alpha-ketoacid as the main component.
The above description is only for the purpose of illustrating the preferred embodiments of the present invention and is not to be construed as limiting the invention, and any modifications, equivalents or improvements made within the spirit and principle of the present invention should be included in the scope of the present invention.

Claims (9)

1. An effervescent tablet comprising an alpha-keto acid, characterized by: the composition comprises the following components in parts by weight:
60-100 parts of alpha-keto acid;
alpha-ketonate 230-410 parts;
20-100 parts of trehalose;
10-60 parts of L-glutamine;
1-10 parts of magnesium aminoacetate;
1-10 parts of carnosine zinc;
1-10 parts of lysine;
1-10 parts of arginine;
5-60 parts of flavoring agent;
wherein the alpha-keto acid comprises alpha-ketoglutaric acid, alpha-hydroxymethionine; the alpha-ketoacid salt comprises alpha-ketovaline calcium, alpha-ketoleucine calcium, alpha-ketoisoleucine calcium, alpha-ketoacid calcium and alpha-ketophenylalanine calcium;
the alpha-keto acid comprises the following components in parts by weight:
20-30 parts of alpha-ketoglutaric acid;
40-70 parts of alpha-hydroxymethionine;
the alpha-ketonic acid salt comprises the following components in parts by weight:
60-90 parts of alpha-ketovaline calcium;
70-120 parts of alpha-ketoleucine calcium;
40-80 parts of alpha-ketoisoleucine calcium;
30-50 parts of alpha-calcium ketoate;
30-70 parts of alpha-ketophenylalanine calcium.
2. The effervescent tablet comprising an α -keto acid of claim 1, wherein: also comprises an alkaline regulator and a binder; wherein the dosage of the adhesive is 2 to 7 percent of the total weight of the other components.
3. The effervescent tablet comprising an α -keto acid of claim 2, wherein: the alkaline regulator is a mixture of sodium bicarbonate and sodium carbonate, and the mass ratio of the sodium bicarbonate to the sodium carbonate is (0.3-0.5): 1.
4. A process for the preparation of an effervescent tablet comprising an α -keto acid as claimed in any one of claims 1 to 3, characterized in that: at least comprises the following steps:
(1) mixing the trehalose, alpha-keto acid salt, L-glutamine, aminoacetic acid and carnosine zinc, and then carrying out wet granulation to obtain a complex A;
(2) mixing lysine, arginine and a flavoring agent, and then granulating by a wet method to obtain a complex B;
(3) respectively taking part of the complex A and the complex B according to the same weight ratio to prepare aqueous solution, adding an alkaline regulator into the aqueous solution, regulating the pH value to 7.35-7.45, and recording the proportion of the alkaline regulator to the complex A and the complex B;
(4) mixing the rest complex A, the rest complex B and an alkaline regulator according to the proportion in the step (3) to obtain a mixed material;
(5) uniformly spraying a binding agent with the weight of 2-7% of the total weight of the mixed material into the mixed material, and tabletting to obtain the effervescent tablet containing the alpha-ketoacid.
5. The method of preparing an effervescent tablet comprising an α -keto acid as claimed in claim 4, wherein: in the mixed material in the step (4), the total weight percentage of the alpha-ketonic acid and the alpha-ketonate is 40-70% by taking the total weight of the mixed material as 100%.
6. The method of preparing an effervescent tablet comprising an α -keto acid as claimed in claim 4, wherein: in the steps (1) and (2), the mixing treatment is realized by a mixer; the mixer is a double-cone or V-cone mixer.
7. The method of preparing an effervescent tablet comprising an α -keto acid as claimed in any one of claims 4 to 6, wherein: the wet granulation is realized by a granulator, the water for the wet granulation is purified water or deionized water, and the water temperature is 15-25 ℃.
8. The method of preparing an effervescent tablet comprising an α -keto acid as claimed in any one of claims 4 to 6, wherein: the particle size of the complex A is less than or equal to 120 mu m; the particle size of the complex B is less than or equal to 120 mu m.
9. The method of preparing an effervescent tablet comprising an α -keto acid as claimed in any one of claims 4 to 6, wherein: the mass fraction of the aqueous solution is 4%.
CN201710854945.3A 2017-09-20 2017-09-20 Effervescent tablet containing alpha-ketoacid and preparation method thereof Active CN107549803B (en)

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